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Tiplaxtinin

Chemical Structure : Tiplaxtinin

CAS No.: 393105-53-8

Tiplaxtinin (PAI-039, PAI 039)

Catalog No.: PC-49768Not For Human Use, Lab Use Only.

Tiplaxtinin (PAI-039) is a selective, orally active plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 uM and Kd of 0.48 uM.

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Biological Activity

Tiplaxtinin (PAI-039) is a selective, orally active plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 uM and Kd of 0.48 uM.
Tiplaxtinin (PAI-039) exhibited in vivo oral efficacy in models of acute arterial thrombosis.
Tiplaxtinin (PAI-039) inhibited PAI-1 and accelerated fibrinolysis while maintaining normal coagulation in a model of coronary occlusion.
Tiplaxtinin (PAI-039) significantly attenuated Ang II-induced aortic medial and wall thickening, enhanced Ang II/salt-induced cardiac fibrosis.
Tiplaxtinin (PAI-039) effectively protected from L-NAME-induced thrombosis in murine model of hepatic vein thrombosis.

Physicochemical Properties

M.Wt 439.39
Formula C24H16F3NO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

{1-benzyl-5-[4-(trifluoromethoxy)phenyl]-1H-indol-3-yl}(oxo)acetic acid

References

1. Weisberg AD, et al. Arterioscler Thromb Vasc Biol. 2005 Feb;25(2):365-71.

2. Elokdah H, et al. J Med Chem. 2004 Jul 1;47(14):3491-4.

3. Hennan JK, et al. J Pharmacol Exp Ther. 2005 Aug;314(2):710-6.

4. Smith LH, et al. Blood. 2006 Jan 1;107(1):132-4.

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